Estrogens play an important role in the growth, development and maintenance of a variety of tissues which are mainly mediated by the estrogen receptor (ER), a ligand-activated nuclear receptor transcription factor. There are two distinct subtypes of estrogen nuclear receptors, ERα and ERβ, which are found to diverge with respect to their transcriptional activities and tissue distribution. ERβ is a target for agonist-based drug leads to treat a wide range of indications, including depression, anxiety and dementia. In contrast, ERα activity can present risks for cancer. 4-Cycloheptyl- and 4-cyclohexylphenols (1 and 2 respectively) were previously found to be potent and highly selective ERβ agonists. The synthesis and evaluation of 4-cyclopentylphenols (3) as ER agonists will be presented.

Synthesis and evaluation of 4-(cyclopentyl)phenols as estrogen receptor agonists

ACS Spring 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.